JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
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2022
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IF 1.61
Wei-Wei Ye,Xiang-Ying Meng,Qian Zhao,Jian-Yang Chen,Cong Liu,Feng Chen,Yong Zhou,Yi Wang
Echinacoside (ECH) is the main compound of Cistanche deserticola, which possesses antioxidant, antitumor, antifatigue, and anti-inflammatory properties. The present study investigated the protective effects of echinacoside on type 2 diabetes mellitus (T2DM)-induced injury in T2DM injury db/db mice model and insulin-resistant LO2 cell model. The results demonstrated that ECH probably alleviated T2DM-induced injury by mediating the AKT pathway, which provided a new direction for the treatment of T2DM-induced injury.
研究领域:
药理学
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糖尿病研究
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细胞生物学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2023
·
IF 5.4
Jiao Wei,Zongmei Zheng,Xinxin Hou,Fengjing Jia,Yuan Yuan,Fuwen Yuan,Feng He,Liang Hu,Ling Zhao
Ethnopharmacological relevance Echinacoside (ECH) is the dominant phenylethanoid glycoside-structured compound identified from our developed herbal formula Huangci granule, which has been previously reported to inhibit the invasion and metastasis of CRC and prolong patients’ disease-free survival duration. Though ECH has inhibitory activity against aggressive colorectal cancer (CRC) cells, its anti-metastasis effect in vivo and the action mechanism is undetermined. Given that ECH has an extremely low bioavailability and gut microbiota drives the CRC progression, we hypothesized that ECH could inhibit metastatic CRC by targeting the gut microbiome . Aim of the study The purpose of this study was to investigate the impact of ECH on colorectal cancer liver metastasis in vivo and its potential mechanisms. Materials and methods An intrasplenic injection-induced liver metastatic model was established to examine the efficiency of ECH on tumor metastasis in vivo . Fecal microbiota from the model group and the ECH group were separately transplanted into pseudo-sterile CRLM mice in order to verify the role of gut flora in the ECH anti-metastatic effect. The 16S rRNA gene sequence was applied to analyze the structure and composition of the gut microbiota after ECH intervention, and the effect of ECH on short-chain fatty acid (SCFAs)-producing bacteria growth was proven by anaerobic culturing in vitro . GC-MS was applied to quantitatively analyze the serum SCFAs levels in mice. RNA-seq was performed to detect the gene changes involving tumor-promoting signaling pathway. Results ECH inhibited CRC metastasis in a dose-dependent manner in the metastatic colorectal cancer (mCRC) mouse model. Manipulation of gut bacteria in the mCRC mouse model further proved that SCFA-generating gut bacteria played an indispensable role in mediating the antimetastatic action of ECH. Under an anaerobic condition, ECH benefited SCFA-producing microbiota without affecting the total bacterial load, presenting a dose-dependent promotion on the growth of a butyrate producer, Faecalibacterium prausnitzii ( F.p ). Furthermore, ECH-reshaped or F.p -colonized microbiota with a high butyrate-producing capability inhibited liver metastasis by suppressing PI3K/AKT signaling and reversing the epithelial-mesenchymal transition (EMT) process, whereas this anti-metastatic ability was abrogated by the butyrate synthase inhibitor heptanoyl-CoA. Conclusion This study demonstrated that ECH exhibits oral anti-metastatic efficacy by facilitating butyrate-producing gut bacteria, which downregulates PI3K/AKT signaling and EMT. It hints at a novel role for ECH in CRC therapy.
研究领域:
药理学
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肿瘤学
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微生物学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2025
·
IF 8.3
Li Fan,Jian Liu,Lin Li,Xueping Yang,Qingwei Zhao,Lijuan Zhao
Background Echinacoside (ECH), a natural phenylethanoid glycoside, has demonstrated protective effects against type 2 diabetes mellitus (T2DM). However, the mechanism underlying the low bioavailability yet advantageous anti-diabetic of ECH remains unresolved. Purpose To elucidate the mechanism of ECH against T2DM through gut microbiota-mediated host metabolism for the first time. Study design and methods A T2DM mouse model was established using a high-fat diet in combination with streptozotocin injection. The therapeutic effects of ECH against T2DM were evaluated by measuring fasting blood glucose (FBG), insulin resistance, glucose intolerance, blood lipids and organ damage in mice. Fecal 16S rRNA and ITS sequencing techniques were employed to characterize the composition of gut microbiota, followed by analysis of bacterial-fungal trans-kingdom network. Metabolomics was conducted to assess the ECH-induced metabolite profile alterations. Additionally, the predicted mechanism of ECH on T2DM was investigated through measuring the hepatic gluconeogenesis markers and inflammation by western blotting, immunohistochemistry, enzymatic assays and antimicrobial mixture (ABX) experiments. Results ECH exhibited significant protective effects against T2DM, as evidenced by reductions in FBG and fasting insulin levels, improvements in glucose and insulin tolerance, attenuations of hyperlipidemia, and alleviation of liver, kidney, and colon damage in T2DM mice. Furthermore, ECH modulated gut microbiota by decreasing the abundances of conditional pathogenic intestinal bacteria ( Klebsiella and Escherichia-Shigella ) and fungi ( Debarymoyces ), while increasing beneficial bacteria ( Lactobacillus ) and fungi ( Wallemia and Penicillium ). Moreover, ECH could restore the disrupted trans-kingdom network between gut fungi and bacteria, thereby suppressing the inflammation-mediated hepatic gluconeogenesis via downregulation of FBP1, PCK1 and G6PC expression. Correspondingly, ABX experiments indicated that once the regulatory function of gut microbiota imbalance was blocked, the anti-T2DM effects of ECH were weakened, accompanied by a failure to improve the levels of inflammation and key gluconeogenic markers in T2DM mice. Conclusion This study presents novel evidence indicating that ECH alleviates T2DM through inhibiting hepatic gluconeogenesis via gut bacterial-fungal trans-kingdom network reconstruction. These findings suggest that ECH may serve as a promising therapeutic strategy for T2DM management, providing new insights for the prevention and treatment of clinical diabetes and its complications.
研究领域:
医学
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微生物学
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代谢组学
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产品关联
DOI
PubMed
高影响因子
PHYTOCHEMICAL ANALYSIS
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2021
·Vol. 32
·期 6
·1074-1081
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IF 3.373
Yanfang Wu,Yindi Chu,Qinyu Yang,Mengjia Li,Miao Yu,Ruixue Deng,Kun Liu,Xinsheng Wang,Enguo Fan
Introduction Syringa pubescens Turcz. was reported to be abundant in the Funiu Mountains of Henan Province and can be used to treat hepatitis and cirrhosis. In order to develop and utilise the resource, a fast and simple technique to extract bioactive compounds is needed. Objectives Our aims were to provide an extraction technique of glycosides from S. pubescens and study the antioxidant activity of this material. Methods Box–Behnken design (BBD) was employed with three factors at three levels. The process parameters such as ethanol concentration ( X 1 ), temperature ( X 2 ), and solvent–solid ratio ( X 3 ) could significantly influence efficiency and yield of target compounds. High-performance liquid chromatography (HPLC) was used to determine the content of glycosides. DPPH (α,α-diphenyl-β-picrylhydrazyl), ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) and reducing power were used to evaluate the antioxidant activity of S. pubescens extract. Results The optimal parameters for the maximal extraction yield were obtained with ethanol concentration of 68%, temperature of 89°C, solvent–solid ratio of 46 mL/g, and time of 20 min. The S. pubescens extract showed strong antioxidant properties in vitro . Conclusion The findings indicated the potential application of solvothermal extraction method to extract bioactive compounds from S. pubescens Turcz. Furthermore, the S. pubescens extract could be used as an important resource of antioxidant activity.
研究领域:
植物化学
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药用植物学
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天然产物化学
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产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
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2018
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IF 3.457
Min Chen,Xiaodong Wang,Bo Hu,Jian Zhou,Xin Wang,Wei Wei,Hua Zhou
Echinacoside is a natural ingredient with various pharmacological activities . In this study, we investigated the protective effects of echinacoside on cardiomyocytes (rat H9c2 cells) in an anoxia/reperfusion (A/R) model. Further, the regulatory function of sodium-calcium exchanger protein 3 (SLC8A3/NCX3) as well as the protein kinase B (AKT) signaling were studied. The present results indicated that echinacoside protected against A/R-induced apoptosis in a dose manner, which was characterized by a decrease in the apoptosis and caspase 3 protein levels in H9c2 cells. Further, Ca 2+ uptake were dose-dependently reduced in H9c2 cells by echinacoside under A/R conditions. Whereas, relative mRNA expression of SLC8A3 and protein levels of SLC8A3 and p-AKT showed opposite tendency. On the one hand, the A/R-induced abnormalities in H9c2 cells were remarkably ameliorated by activated p-AKT and over-expression of SLC8A3 but aggravated by inhibited p-AKT, and the aggravated effection were ameliorated by echinacoside. Moreover, protein levels of SLC8A3 were positively regulated by p-AKT signaling. On the other hand, apoptosis and Ca 2+ uptake as well as protein levels of caspase 3 were significantly increased by SLC8A3 silencing in H9c2 cells under normoxic conditions, and this symptom was remarkably reversed by echinacoside or Nimodipine (an antagonis of Ca 2+ ) treatment . Collectively, echinacoside has showed a cardioprotective effect against A/R treatment in a dose dependent manner in vitro, and this cardioprotective effect was potentially achieved via up-regulating p-AKT and SLC8A3.
研究领域:
药理学
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心脏病学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2015
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IF 2.912
Yang Li,Guisheng Zhou,Shihua Xing,Pengfei Tu,Xiaobo Li
Echinacoside (ECH) is one of the representative phenylethanoid glycosides. It is widely present in plants and exhibits various bioactivities. However, the extremely low oral bioavailability of ECH in rats implies that ECH may go through multiple hydrolysis steps in the gastrointestinal tract prior to its absorption into the blood. Therefore, the gastrointestinal metabolites of ECH are more likely to be the bioactive components. This study established an approach combining ultraperformance liquid chromatography–quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) with MSE technology and MetaboLynx software for rapid analysis of the ECH metabolic profile produced by human intestinal bacteria. As a result, 13 ECH metabolites and 5 possible metabolic pathways (including deglycosylation, dehydroxylation, reduction, hydroxylation, and acetylation) were identified. Furthermore, hydroxytyrosol (HT) and 3-hydroxyphenylpropionic acid (3-HPP) were found to be the two bioactive metabolites of ECH produced by human intestinal bacteria.
研究领域:
药理学
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微生物学
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分析化学
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产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING RESEARCH & DESIGN
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2022
·
IF 4.119
Chunying Li,Fang Nie,Changyin Feng,Mengfei Tian,Meiting Yu,Chunjian Zhao,Yujie Fu
A creative dual-template molecularly imprinted polymer (Fe 3 O 4 @MCM-41-MIPs) with good magnetic properties and specific recognition of echinacoside and acteoside was prepared by surface imprinting. Echinacoside and acteoside served as dual templates, 4-vinylpyridine (4-VP) was used as a functional monomer , the cross-linker was ethylene glycol dimethacrylate (EGDMA), and the selected initiator was azobisisobutyronitrile (AIBN). The prepared Fe 3 O 4 @MCM-41-MIPs were applied to the selective separation and enrichment of echinacoside and acteoside from Cistanche deserticola Y. C. Ma ( C. deserticola ). The resulting Fe 3 O 4 @MCM-41-MIPs were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), laser particle size scanning and vibration sample magnetometry (VSM). The results of the isotherm adsorption experiment showed that the maximum adsorption capacities of Fe 3 O 4 @MCM-41-MIPs for echinacoside and acteoside were 6.02 and 1.63 mg·g -1 , respectively, at 298 K. The pseudo-second-order reaction mechanism showed that the equilibrium adsorption capacities of Fe 3 O 4 @MCM-41-MIPs for echinacoside and acteoside were 4.81 and 0.93 mg·g -1 , respectively. The characterization of Fe 3 O 4 @MCM-41-MIPs showed that the imprinted layer with dual-template molecules was wrapped on the outside of the carrier, and the obtained Fe 3 O 4 @MCM-41-MIPs showed good saturation magnetization , desirable capacity for echinacoside and acteoside adsorption, and satisfactory reuse (echinacoside and acteoside maintained relative adsorption rates of 97.5% and 95.8% after five cycles). After separation, the purities of echinacoside and acteoside were 33.50% and 27.00%, respectively. In addition, in the selective adsorption experiment, the synthesized Fe 3 O 4 @MCM-41-MIPs showed better selectivity for echinacoside and acteoside than their structural analogs. Therefore, this method proved to be sustainable, rapid and highly efficient for the separation and enrichment of echinacoside and acteoside.
研究领域:
中药化学
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分离科学
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产品关联
DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2020
·
IF 3.69
Yi Chen,Ying-Qi Li,Jia-Yi Fang,Ping Li,Fei Li
Ethnopharmacological relevance Cistanche tubulosa is a precious traditional Chinese medicine that has been widely used in the treatment of osteoporosis and Alzheimer's disease . Echinacoside and acteoside are the main active constituents in Cistanche tubulosa that have the pharmacological activities with research value. It has been reported that echinacoside and acteoside could improve the learning and memory ability, promote the proliferation and differentiation of osteoblast. Aim of study Echinacoside and acteoside from Cistanche tubulosa have shown significant activities of anti-osteoporosis and anti-Alzheimer's disease, while these effects have not been studied concurrently in a rat model. The aim of this study was to establish and verify the model of osteoporosis combined with Alzheimer's disease in rat, and to investigate the double effects of echinacoside and acteoside on this concurrent model. Materials and methods Three model groups of ovariectomy (OVX), sham surgery with D-galactose and AlCl 3 (D), ovariectomy with D-galactose and AlCl 3 (OVX + D) were set at the same time. The rats in drug treatment groups were ovariectomized. While conducting the intraperitoneal injection of D-galactose and intragastric administration of AlCl 3 in the rats of drug treatment groups, the rats were orally administered echinacoside (90 mg/kg/d), acteoside (90 mg/kg/d) and the positive control drugs of estradiol valerate (0.6 mg/kg/d), donepezil HCl (0.8 mg/kg/d), respectively. After the drug treatment of 8 weeks, Morris Water Maze (MWM) test for 6 days was firstly performed. The rats were then sacrificed to harvest the blood, uteri, femora, tibiae and brain tissues. The serum was used for biochemical tests. The uteri were used for histomorphometry. The right femora were used for Micro-CT and histomorphometry, respectively. The right tibiae were used for biomechanical test. The hippocampus collected on ice box was used for biochemical tests. The brain collected by perfusion was used for histomorphometry. Results Compared with Sham group, OVX + D group could significantly reduce the learning and memory ability by causing oxidative damage, impairing neurons in hippocampus and affecting the hydrolysis and synthesis of acetylcholine . Meanwhile, the activities of BALP and TRAP in OVX + D group increased significantly ( P < 0.001) as compared to Sham group. In addition, compared with Sham group, the mean bone mineral density obviously decreased ( P < 0.05), the trabecular bone mass and microarchitecture were also destroyed significantly in OVX + D group. Furthermore, the maximum load and maximum stress significantly reduced ( P < 0.01) and the energy absorption also decreased greatly as compared to Sham group. After administrated with echinacoside and acteoside, the typical pathological features of osteoporosis and Alzheimer's disease were ameliorated. Conclusions The model of osteoporosis combined with Alzheimer's disease in rat was feasible and successfully established. Echinacoside and acteoside also showed some significant effects on this concurrent model, and they could be potential candidates from Cistanche tubulosa with double effects for further study.
研究领域:
药理学
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神经科学
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老年医学
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DOI
PubMed
高影响因子
ACS Omega
·
2023
·
IF 4.1
Yi Chen,Yongfang Wang,Shasha Song,Xiaoli Zhang,Lili Wu,Jianbing Wu,Xinyu Li
Baicalin (BAI), the main active component of Scutellaria baicalensis, has significant anti-inflammatory and antibacterial effects. Echinacoside (ECH), an active component from Echinacea purpurea, has significant antiangiogenesis and antioxidant effects. In previous studies, BAI or ECH has been used for some skin inflammation problems by topical treatment. Psoriasis (PSO) is a common inflammatory skin disease with typical features such as excessive inflammatory response and vascular proliferation in skin lesions. Because of the anti-inflammatory effect of BAI and the antiangiogenic activity of ECH, it is proposed that the combination of BAI and ECH can ameliorate psoriatic skin lesions better than a single component. This study aims to explore the effects and potential mechanisms of BAI combined with ECH on imiquimod (IMQ)-induced psoriatic skin lesions by topical treatment. Transcriptome analysis first showed that the TNF signaling pathway and the VEGF signaling pathway were significantly enriched in IMQ-induced psoriatic skin lesions. Topical application of BAI combined with ECH could ameliorate IMQ-induced skin lesions in mice, especially the better effects of B2-E1 (BAI/ECH = 2:1). Network pharmacology analysis and molecular docking indicated that BAI-treated PSO on the skin by regulating the TNF signaling pathway, and ECH treated PSO on the skin by regulating the VEGF signaling pathway. Meanwhile, the ELISA test and the qPCR assay showed that BAI combined with ECH could inhibit the expression of key cytokines and genes related to the TNF signaling pathway and the VEGF signaling pathway. Zebrafish experiments demonstrated the anti-inflammatory and antiangiogenic effects of BAI combined with ECH and revealed the potential mechanisms associated with regulating the inflammation-related TNF signaling pathway and the angiogenesis-related VEGF signaling pathway. This suggested that BAI combined with ECH may be a promising topical agent to ameliorate psoriatic skin lesions in the future.
研究领域:
药理学
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皮肤病学
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分子生物学
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炎症研究
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血管生成研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）